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Microbiology

Repression of HIV-1 reactivation mediated by CRISPR/dCas9-KRAB in lymphoid and myeloid cell models

8 | Jun 26 2022

Lendel Correia da Costa et al. demonstrated that KRAB repressor protein was crucial to reactivation resistance phenotype. [Read the Full Post]

Histone Deacetylase Inhibitors Counteract CGRP Signaling and Pronociceptive Sensitization in a Rat Model of Medication Overuse Headache

8 | Jun 26 2022

Matteo Urru et al. provided evidence for a key role of HDACs and epigenetics in MOH pathogenesis, highlighting the therapeutic potential of HDAC inhibition in the prevention of migraine chronification. [Read the Full Post]

The PRC2 molecule EED is a target of epigenetic therapy for neuroblastoma

15 | Jun 23 2022

Dilibaerguli Shaliman et al. suggested that inhibitory cell cycle-regulated gene sets were markedly up-regulated. [Read the Full Post]

Real-world experience in treating pediatric relapsed/refractory or therapy-related myeloid malignancies with decitabine, vorinostat, and FLAG therapy based on a phase 1 study run by the TACL consortium

14 | Jun 22 2022

Eric S Schafer et al. found that therapy was well tolerated and effective in pediatric patients with R/R myeloid neoplasms, particularly those with epigenetic alterations, t-AML, and refractory disease. [Read the Full Post]

Three Birds, One Excipient: Development of an Improved pH, Isotonic, and Buffered Ketamine Formulation for Subcutaneous Injection

38 | Jun 03 2022

Jason Wallach et al. found that this strategy has the potential to be readily adapted to other amine-based APIs. [Read the Full Post]

Stability of Captisol-enabled versus propylene glycol-based melphalan at room temperature and after refrigeration

32 | Jun 03 2022

Jitesh D Kawedia et al. found that CE-melphalan at 2 mg/mL has 24-hour stability at RT and can be used for extended infusion times or may be compounded ahead of time. Reconstituted CE-melphalan vials are stable for 48 hours at both RT and 4 °C. [Read the Full Post]

Physicochemical Characterization, Molecular Docking, and In Vitro Dissolution of Glimepiride-Captisol Inclusion Complexes

42 | Jun 01 2022

Arpita Pal et al. found that complexation with Captisol enhanced the water solubility of glimepiride. [Read the Full Post]

Evaluation of mitochondrial oxidative toxicity in mammalian cardiomyocytes by determining the highly reproducible and reliable increase in mitochondrial superoxides after exposure to therapeutic drugs

95 | May 27 2022

Dohee Ahn et al. found that a screening system using MitoSOX™ had the potential to be applied as a reliable biomarker for determining mitochondrial oxidative toxicity in new drug development. [Read the Full Post]

COVID-19: Implications Regarding the Properties and Behaviors of the Coronavirus Disease

73 | May 14 2022

COVID-19 may be inaccurate due to errors in diagnosing and reporting, since other similar illnesses may exhibit similar symptoms. [Read the Full Post]

The Mycotoxin Beauvericin Exhibits Immunostimulatory Effects on Dendritic Cells via Activating the TLR4 Signaling Pathway

88 | May 10 2022

Xiaoli Yang et al. identified TLR4 as a cellular BEA sensor and define BEA as a potent activator of BMDCs, implying that this compound could be exploited as a promising candidate structure for vaccine adjuvants or cancer immunotherapies. [Read the Full Post]

[Ocular toxicity of targeted therapies with MEK inhibitors and BRAF inhibitors in the treatment of metastatic cutaneous melanoma]

90 | May 06 2022

E Fauviaux et al. found that a multidisciplinary approach including ophthalmologists, dermatologists and oncologists was essential in order to adapt treatment in the advent of the ocular complications. [Read the Full Post]

Alternating therapy with osimertinib and afatinib for treatment-naive patients with EGFR-mutated advanced non-small cell lung cancer: A single-group, open-label phase 2 trial (WJOG10818L)

109 | May 02 2022

Hidetoshi Hayashi et al. found that Alternating therapy with osimertinib and afatinib for treatment-naive patients with EGFR- mutated advanced NSCLC did not meet its primary end point, despite the encouraging efficacy and safety profile of this treatment strategy. [Read the Full Post]

Clinically relevant CHK1 inhibitors abrogate wild-type and Y537S mutant ERα expression and proliferation in luminal primary and metastatic breast cancer cells

165 | Apr 20 2022

Sara Pescatori et al. thought that CHK1 could be considered as an appealing novel pharmacological target for the treatment of luminal primary and MBCs. [Read the Full Post]

Factors Influencing the Intracellular Concentrations of the Sofosbuvir Metabolite GS-331007 (in PBMCs) at 30 Days of Therapy

161 | Apr 02 2022

Jessica Cusato et al. presented data on an IC evaluation in a cohort of patients treated with SOF, also considering pharmacogenetics. [Read the Full Post]

Drug repurposing through virtual screening and in vitro validation identifies tigecycline as a novel putative HCV polymerase inhibitor

132 | Apr 01 2022

Mahmoud ElHefnawi et al. found that tigecycline displayed synergistic activity with sofosbuvir and daclatasvir against HCV. [Read the Full Post]

SC75741, A Novel c-Abl Inhibitor, Promotes the Clearance of TDP25 Aggregates via ATG5-Dependent Autophagy Pathway

95 | Feb 26 2022

Dongheng Zhou et al. found that dual-targeted inhibition of c-Abl and NF-κB may be a potential treatment for TDP43 proteinopathies and ALS. [Read the Full Post]

Baricitinib for relapsing giant cell arteritis: a prospective open-label 52-week pilot study

274 | Feb 23 2022

Matthew J Koster et al. showed that in this proof-of-concept study, baricitinib at 4 mg/day was well tolerated and discontinuation of GC was allowed in most patients with relapsing GCA. [Read the Full Post]

Predictors of Treatment Response and Long-Term Outcomes in Young Children with Steroid-Dependent Nephrotic Syndrome Treated with High-Dose Mizoribine as First-Line Steroid-Sparing Agent

109 | Feb 23 2022

Shuichiro Fujinaga et al. discovered that high-dose mizoribine might be an attractive treatment option as initial SSA in young children with low steroid-dependent dose for improved long-term outcomes. [Read the Full Post]

Drug survival of biologics and novel immunomodulators for rheumatoid arthritis, axial spondyloarthritis, psoriatic arthritis, and psoriasis - A nationwide cohort study from the DANBIO and DERMBIO registries

210 | Feb 22 2022

Alexander Egeberg et al. emphasized that although these diseases had many overlaps in their pathogenesis, there was a need for an individualized treatment approach that considered the underlying disease, patient profile, and treatment history. [Read the Full Post]

Screening of the ubiquitin-proteasome system activators for anti-Alzheimer's disease by the high-content fluorescence imaging system

0 | Feb 03 2022

Yi-Ling Wang found that a novel insight into the discovery and development of anti-AD drugs. [Read the Full Post]

A standard knockout procedure alters expression of adjacent loci at the translational level

143 | Feb 02 2022

Artyom A Egorov et al. estimated that in as much as ∼1/5 of knockout strains the expression of neighboring genes might be substantially (>2-fold) deregulated at the level of translation. [Read the Full Post]

Drug repositioning based on gene expression data for human HER2-positive breast cancer

208 | Jan 21 2022

Farkhondeh Khanjani et al. suggested that some repurposed drugs based on gene expression data could be noticed as potential drugs for the treatment of HER2-positive breast cancer. [Read the Full Post]

Integrated Genomic Profiling and Drug Screening of Patient-Derived Cultures Identifies Individualized Copy Number-Dependent Susceptibilities Involving PI3K Pathway and 17q Genes in Neuroblastoma

143 | Jan 20 2022

Rachel L Y Wong et al. defined individualized dose-dependent relationships between copy number gains of PI3K and STAT family genes particularly on 17q and susceptibility to PI3K and cell cycle agents in neuroblastoma. [Read the Full Post]

Differential time course of glycogen synthase kinase-3 inhibition in experimental autoimmune encephalomyelitis

263 | Dec 29 2021

A S Al-Zaidi et al. found that downregulation of Th1 and Th17 hallmark cytokines by Tideglusib in EAE might be associated with IL-10 production. [Read the Full Post]

Small Dense Low-Density Lipoprotein Cholesterol and Cardiovascular Risk in Statin-Treated Patients with Coronary Artery Disease

302 | Dec 28 2021

Junnichi Ishii et al. investigated the relationship between small dense low-density cholesterol (sdLDL-C) and risk of major adverse cardiovascular events (MACE) in patients treated with high- or low-dose statin therapy. [Read the Full Post]

A nephroprotective iodinated contrast agent with cardioprotective properties: A pilot study

325 | Nov 13 2021

Elizabeth S Rowe et.al suggested that SBECD-iohexol is superior to iohexol alone, for both the preservation of cardiomyocyte integrity and preservation of myocardial function in myocardial ischemia. [Read the Full Post]

Dual PI3K/mTOR inhibitor NVP‑BEZ235 decreases the proliferation of doxorubicin‑resistant K562 cells

1189 | Oct 17 2021

Jie Li et al. suggested that BEZ235 might reverse Doxo resistance in leukemia cells. [Read the Full Post]

Targeting mTOR signaling overcomes acquired resistance to combined BRAF and MEK inhibition in BRAF-mutant melanoma

586 | Oct 17 2021

Beike Wang et al. revealed that mTOR activation was essential for drug resistance of melanoma to MAPK inhibitors, and provided insight into the rewiring of the signaling networks in CR melanoma. [Read the Full Post]

A [3Fe-4S] cluster and tRNA-dependent aminoacyltransferase BlsK in the biosynthesis of Blasticidin S

477 | Oct 03 2021

Xiankun Wang et al. provided an example of an iron-sulfur protein that catalyzed an aminoacyl-tRNA (aa-tRNA)-dependent amide bond formation in a natural product biosynthetic pathway. [Read the Full Post]

EGFR and ERK activation resists flavonoid quercetin-induced anticancer activities in human cervical cancer cells in vitro

471 | Sep 21 2021

Xin Chen et al.determined the role of EGFR and the underlying signaling pathways involved in the anti-cervical cancer malignant behavior induced by Que and identified the negative regulatory association. [Read the Full Post]

Identification of FDA approved drugs against SARS-CoV-2 RNA dependent RNA polymerase (RdRp) and 3-chymotrypsin-like protease (3CLpro), drug repurposing approach

213 | Sep 08 2021

Zahra Molavi et al. recommended further experimental evaluations in vitro and in vivo on FDA-approved drugs to assess their potential antiviral effect on SARS-CoV-2. [Read the Full Post]

Impact of FasL Stimulation on Sclerostin Expression and Osteogenic Profile in IDG-SW3 Osteocytes

471 | Aug 30 2021

Adela Kratochvilova et al. found the caspase-independent impact of FasL stimulation. [Read the Full Post]

ARTEMIN Promotes Oncogenicity and Resistance to 5-Fluorouracil in Colorectal Carcinoma by p44/42 MAPK Dependent Expression of CDH2

619 | Aug 25 2021

Qiu-Shi Zhuang et al. thought that ARTN might be of prognostic and theranostic utility in CRC. [Read the Full Post]

Tofacitinib Ameliorates Lupus Through Suppression of T Cell Activation Mediated by TGF-Beta Type I Receptor

812 | Aug 20 2021

Qing Yan et al. thought that tofacitinib could suppress T cell activation by upregulating TGFβRI expression, which provided a possible molecular mechanism underlying clinical efficacy of tofacitinib in treating SLE patients. [Read the Full Post]

Sinus rhythm heart rate increase after atrial fibrillation ablation is associated with lower risk of arrhythmia recurrence

613 | Aug 11 2021

Ammar M Killu et al. showed that relative changes in HR post AF ablation correlates with AF recurrence. [Read the Full Post]

Efficacy and Safety of Emricasan in Liver Cirrhosis and/or Fibrosis

495 | Aug 10 2021

Li-Ya Mu et al. found that treatment with emricasan was more effective in improving liver function and apoptosis parameters compared to placebo, with a well-tolerated safety profile. [Read the Full Post]

Local ablation of gastric cancer by reconstituted apolipoprotein B lipoparticles carrying epigenetic drugs

820 | Aug 03 2021

Chia-Lung Yang et al. established rABL-based nanoparticles embedded epigenetic inhibitors for local treatment of gastric cancer, which had good therapeutic effects but do not cause severe side effects. [Read the Full Post]

High-Throughput Mechanistic Screening of Epigenetic Compounds for the Potential Treatment of Meningiomas

832 | Aug 02 2021

Philip D Tatman et al. suggested an important role of HDACs in meningioma biology and as a targetable mechanism. [Read the Full Post]

Effect of Decitabine (5-aza-2'-deoxycytidine, 5-aza-CdR) in Comparison with Vorinostat (Suberoylanilide Hydroxamic Acid, SAHA) on DNMT1, DNMT3a and DNMT3b, HDAC 1-3, SOCS 1, SOCS 3, JAK2, and STAT3 Gene Expression in Hepatocellular Carcinoma HLE and LCL-PI 11 Cell Lines

598 | Jul 31 2021

Masumeh Sanaei et al. found that 5-Aza-CdR and SAHA could induce cell growth inhibition and apoptosis induction through the JAK/STAT pathway. [Read the Full Post]

Successful Treatment of a Locally Recurrent and Metastatic Malignant Phyllodes Tumor with Accelerated Radiotherapy and Nab-Paclitaxel, Cisplatin, and Liposomal Doxorubicin Chemotherapy

878 | Jul 08 2021

Ioannis M Koukourakis et al. found that the combination of cisplatin with nab-paclitaxel and liposomal doxorubicin chemotherapy had acceptable toxicity and was highly effective in eradicating metastatic lesions. [Read the Full Post]

Allosteric Activation of SARS-CoV-2 RNA-Dependent RNA Polymerase by Remdesivir Triphosphate and Other Phosphorylated Nucleotides

471 | Jun 23 2021

Bing Wang et al. demonstrated that RdRp was allosterically activated by nontemplating phosphorylated nucleotides, including naturally occurring alarmone ppGpp and synthetic remdesivir triphosphate. [Read the Full Post]

HeLa TI cell-based assay as a new approach to screen for chemicals able to reactivate the expression of epigenetically silenced genes

562 | Jun 18 2021

Varvara Maksimova et al. showed that N-nitrosodiphenylamine and N-nitrosodimethylamine reactivated epigenetically silenced genes, probably by affecting DNA methylation. [Read the Full Post]

Real-world-evidence-for-carfilzomib-dosing-intensity-on-overall-survival-and-treatment-progression-in-multiple-myeloma-patients

597 | Jun 13 2021

Noopur Raje found that patient outcomes could be improved if eligible MM patients are treated with the optimized [Read the Full Post]

Efficacy of tyrosine kinase inhibitors against lung cancer with EGFR exon 18 deletion: Case report and pooled analysis

805 | Jun 08 2021

Rafael Rubiera-Pebe et al. showed that afatinib was associated with a greater tumor response rate and a longer PFS than the first generation TKIs. [Read the Full Post]

Treatment of Luminal Metastatic Breast Cancer beyond CDK4/6 Inhibition: Is There a Standard of Care in Clinical Practice?

988 | May 21 2021

Athanasios Mavratzas et al. thought that treatment of metastatic luminal breast cancer after progression on CDK4/6 inhibitors remained a challenge. [Read the Full Post]

In vitro antiviral activity of the anti-HCV drugs daclatasvir and sofosbuvir against SARS-CoV-2, the aetiological agent of COVID-19

480 | Apr 22 2021

Carolina Q Sacramento et al. found that daclatasvir, alone or in combination with sofosbuvir, at higher doses than used against HCV, might be further fostered as an anti-COVID-19 therapy. [Read the Full Post]

Naturally Occurring Resistance Associated Substitutions in Non-Cirrhotic, Treatment Naive HCV-HIV Co-Infected Patients Does Not Affect the Treatment Response for Anti-HCV Antiviral Therapy

473 | Apr 22 2021

Ekta Gupta et al. showed that BL-RAS were common in HCV-HIV co-infected patients. [Read the Full Post]

Effect of Eriocalyxin B on prostatic inflammation and pelvic pain in a mouse model of experimental autoimmune prostatitis

485 | Mar 08 2021

Li-Gang Zhang et al. suggested that EriB could alleviate the severity of prostatic inflammation and pelvic pain in an EAP mouse model. [Read the Full Post]

Immediate Effect of Baricitinib on Arthritis and Biological Disease-Modifying Antirheumatic Drug-Induced Psoriasis-Like Skin Lesions in Two Patients with Rheumatoid Arthritis

588 | Mar 05 2021

Yoshifumi Tada et al. found that baricitinib was initiated because of RA flare and resulted in immediate beneficial effects on arthritis as well as skin lesions. [Read the Full Post]

Comparison of Treatment Effect and Tolerance of the Topical Application of Mizoribine and Cyclosporine A in a Mouse Dry Eye Model

518 | Mar 05 2021

Xiang Lin et al. found that MZR (0.05% in PBS) could be a good competitive product for Restasis because of the comparable treatment effect in dry eye diseases and better ocular tolerability in ocular itch and pain. [Read the Full Post]

In-vitro evaluation of the immunomodulatory effects of baricitinib: implication for COVID-19 therapy

654 | Mar 04 2021

Linda Petrone et al. found that exogenous addition of baricitinib decreased the in-vitro SARS-CoV-2-specific response in COVID-19 patients using a whole-blood platform. [Read the Full Post]

The application of nanoparticles in cancer immunotherapy: Targeting tumor microenvironment

650 | Feb 13 2021

Muyue Yang et al. found that the changes of TME at various stages during tumor development are required to be further elucidated so that more individualized nanoplatforms could be designed. [Read the Full Post]

Selective reactivation of STING signaling to target Merkel cell carcinoma

648 | Feb 13 2021

Wei Liu et al. found that targeted delivery and activation of STINGS162A/G230I/Q266I in tumor cells held great therapeutic promise for the treatment of MCC and many other STING-deficient cancers. [Read the Full Post]

The yeast platform engineered for synthetic gRNA-landing pads enables multiple gene integrations by a single gRNA/Cas9 system

504 | Feb 09 2021

Sihyun Baek et al. demonstrated the effectiveness of a single gRNA-mediated CRISPR platform to build complex metabolic pathways in yeast. [Read the Full Post]

[Altered Splicing in Stable Cell Strains Expressing Mini-hF9 Gene with Nonsense Mutation]

438 | Feb 09 2021

Gang Wang et al. found that the nonsense associated altered splicing (NAS) pathway, which generated alternately spliced transcripts, might be triggered in coagulation factor IX gene with nonsense mutation. [Read the Full Post]

CKAP2L promotes non-small cell lung cancer progression through regulation of transcription elongation

407 | Jan 28 2021

Tiziana Monteverde et al. found that the molecular mechanisms through which CKAP2L, a protein involved in CIN, promoted cancer progression and suggested that its inhibition represented a novel therapeutic strategy in NSCLC. [Read the Full Post]

Identification of hub genes and small molecule therapeutic drugs related to breast cancer with comprehensive bioinformatics analysis

434 | Jan 28 2021

Mingqian Hao et al. identified six hub genes and 29 potential drug candidates for breast cancer. [Read the Full Post]

Ebselen, Disulfiram, Carmofur, PX-12, Tideglusib, and Shikonin Are Nonspecific Promiscuous SARS-CoV-2 Main Protease Inhibitors

471 | Jan 07 2021

Chunlong Ma et al. suggested that these six compounds were nonspecific SARS-CoV-2 Mpro inhibitors and urged the scientific community to be stringent with hit validation. [Read the Full Post]

Repurposing FDA Approved Drugs as JNK3 Inhibitor for Prevention of Neuroinflammation Induced by MCAO in Rats

457 | Jan 06 2021

Zikra Zulfiqar et al. demonstrated that the novel FDA-approved medications attenuate ischemic stroke-induced neuronal degeneration, possibly by inhibiting JNK3. [Read the Full Post]

Effect of mechanochemical inclusion of triamterene into sulfobutylether-β-cyclodextrin and its improved dissolution behavior

381 | Nov 23 2020

Hideko Maeda et al. found that the water apparent solubility of TT could be improved by simple mechanical mixing without organic solvents, and improved bioavailability after oral administration was expected. [Read the Full Post]

Brain exposure of the ATM inhibitor AZD1390 in humans - a positron emission tomography (PET) study

363 | Nov 21 2020

Aurelija Jucaite et al. found the potential of PET microdosing in predicting and guiding dose range and schedule for subsequent clinical studies. [Read the Full Post]

A phase I trial of temsirolimus and erlotinib in patients with refractory solid tumors

585 | Nov 15 2020

Haeseong Park et al. found the he combination of temsirolimus and erlotinib at the RP2D was well tolerated, and the regimen resulted in prolonged disease stabilization in selected patients (NCT00770263). [Read the Full Post]

Optimization and Evaluation of Propolis liposomes as a promising therapeutic approach for COVID-19

406 | Nov 11 2020

Hesham Refaat et al. identified the potential of propolis liposomes as a promising treatment approach against COVID-19. [Read the Full Post]

A phase I study of a dual PI3-kinase/mTOR inhibitor BEZ235 in adult patients with relapsed or refractory acute leukemia

454 | Oct 22 2020

Fabian Lang et al.thought that combined inhibition of PI3K and mTOR inhibited a clinically meaningful driver pathway in a small subset of patients with ALL, with no benefit in patients with AML. [Read the Full Post]

HPV-induced Nurr1 promotes cancer aggressiveness, self-renewal, and radioresistance via ERK and AKT signaling in cervical cancer

423 | Oct 20 2020

Peter Kok-Ting Wan et al. provided that BEZ, but not GSK, could abolish Nurr1-enhanced radioresistance, suggesting its potential value for radiosensitizing CSLCs in the clinical setting. [Read the Full Post]

CTELS: A Cell-Free System for the Analysis of Translation Termination Rate

473 | Sep 28 2020

Kseniya A Lashkevich et al. revealed a transient stalling event at a "leaky" stop codon context, which likely defined the basis of nonsense suppression. [Read the Full Post]

Proliferation of Vascular Smooth Muscle Cells under ox-LDL Is Regulated by Alismatis rhizoma Decoction via InhibitingERK1/2 and miR-17∼92a Cluster Activation

433 | Sep 14 2020

Julian Shen et al. provided the multitarget mechanisms for application of AD in the treatment of atherosclerosis. [Read the Full Post]

Fluvastatin potentiates anticancer activity of vorinostat in renal cancer cells

611 | Sep 10 2020

Kazuki Okubo et al. found that there was a positive feedback cycle among AMPK activation, histone acetylation, and ER stress induction. [Read the Full Post]

Molecular dynamic simulations to investigate the structural impact of known drug resistance mutations on HIV-1C Integrase-Dolutegravir binding

219 | Aug 24 2020

Rumbidzai Chitongo et al. suggested the G140S mutant had the strongest effect on the HIV-1C IN protein structure and Dolutegravir binding. [Read the Full Post]

Identification of MYC as an antinecroptotic protein that stifles RIPK1-RIPK3 complex formation

420 | Aug 16 2020

Daehyeon Seong et al. found that MYC-mediated suppression of necroptosis was a mechanism of necroptosis resistance in cancer, and approaches targeting MYC to induce necroptosis represent an attractive therapeutic strategy for cancer. [Read the Full Post]

Giardia duodenalis induces extrinsic pathway of apoptosis in intestinal epithelial cells through activation of TNFR1 and K63 de-ubiquitination of RIP1 in vitro

393 | Aug 11 2020

Lin Liu et al. suggested that Giardia trophozoite stimulation could activate CASP3/8 signaling pathways via activation of TNFR1 and K63 de-ubiquitination of RIP1 caused by up-regulated expressions of CYLD and A20, and promoted Caco-2 cell apoptosis. [Read the Full Post]

Gemcitabine combined with cisplatin vs. taxane, cisplatin, and fluorouracil in the treatment of locally advanced nasopharyngeal carcinoma: a retrospective case-control study

497 | Aug 04 2020

Y-M Huang et al. showed that the clinical efficacy of the GP regimen combined with CCRT for the treatment of locoregionally advanced NPC might be better than that of the TPF regimen. [Read the Full Post]

Effectiveness and Costs Among Rheumatoid Arthritis Patients Treated with Targeted Immunomodulators Using Real-World U.S. Data

629 | Jul 28 2020

Mahdi Gharaibeh et al. showed that the range of patients who were effectively treated with first-line therapy was higher for certain tumor necrosis factor inhibitors and tocilizumab. [Read the Full Post]

Phase 1 trial of carfilzomib (PR-171) in combination with vorinostat (SAHA) in patients with relapsed or refractory B-cell lymphomas

654 | Jul 16 2020

Beata Holkova et al. showed a decrease in NF-κB activation and an increase in Bim levels in some patients, but these changes did not correlate with clinical response. [Read the Full Post]

Advanced bioinformatics rapidly identifies existing therapeutics for patients with coronavirus disease-2019 (COVID-19)

456 | Jul 15 2020

Jason Kim et al. highlighted the potential use of two bioinformatics technologies to rapidly discover existing therapeutic agents that warranted further investigation for established and emerging disease processes. [Read the Full Post]

Histone Deacetylase Inhibition Prevents the Growth of Primary and Metastatic Osteosarcoma

839 | Jul 07 2020

Jeremy J McGuire et al. provided rationale for clinical trials in osteosarcoma patients using the approved therapies panobinostat or romidepsin. [Read the Full Post]

Combination BET Family Protein and HDAC Inhibition Synergistically Elicits Chondrosarcoma Cell Apoptosis Through RAD51-Related DNA Damage Repair

709 | Jul 06 2020

Songwei Huan et al. disclosed that BET and HDAC inhibition synergistically inhibited cell growth and induced cell apoptosis through a mechanism that involved the suppression of RAD51-related HR DNA repair in chondrosarcoma cells. [Read the Full Post]

18 F-Fluoroestradiol ( 18 F-FES)-PET Imaging in a Phase II Trial of Vorinostat to Restore Endocrine Sensitivity in ER+/HER2- Metastatic Breast Cancer

641 | Jul 01 2020

Lanell M Peterson et al. found that Simultaneous HDACi and AI dosing in patients with cancers resistant to AI alone showed clinical benefit (6+ months without progression) in 4 of 10 evaluable patients. [Read the Full Post]

Imaging Assisted Evaluation of Antitumor Efficacy of a New Histone Deacetylase Inhibitor in the Castration-Resistant Prostate Cancer

619 | Jul 01 2020

Zude Chen et al. provided not only a novel epigenetic approach for prostate cancer therapy but also offering a potential tool, [11C] Martinostat PET/CT imaging, to detect the early phase of prostate cancer and monitor therapeutic effect of CN133. [Read the Full Post]

Sulfobutylether-β-cyclodextrin /5,10,15,20-tetrakis(1-methylpyridinium-4-yl)porphine Nanoassemblies With Sustained Antimicrobial Phototherapeutic Action

436 | Jun 08 2020

Roberto Zagami et al. proposed the design and characterization of a novel nanophototherapeutic based on the trade cyclodextrin CAPTISOL® (sulfobutylether-beta-cyclodextrin, SBE-βCD) and 5,10,15,20-tetrakis(1-methylpyridinium-4-yl)porphine tetrakis(p-toluenesulfonate) (TMPyP) to fabricate efficient biocompatible systems for aPDT. [Read the Full Post]

Cell Cycle Arrest and Apoptosis Are Not Dependent on p53 Prior to p53-dependent Embryonic Stem Cell Differentiation

1000 | Jun 02 2020

Sushil K Jaiswal et al. found that the multiple roles of p53 in cell cycle regulation and apoptosis were first acquired during pluripotent stem cell differentiation. [Read the Full Post]

Effects of the Preparation Method on the Formation of True Nimodipine SBE-β-CD/HP-β-CD Inclusion Complexes and Their Dissolution Rates Enhancement

0 | Mar 31 2020

Semcheddine F et al. showed that all the products exhibited higher dissolution rate than those of the physical mixtures and ND alone, in all mediums. However, the kneading complexes displayed the maximum dissolution rate in comparison with drug and other complexes, confirming the influence of the preparation method on the physicochemical properties of the products. [Read the Full Post]

Effects of the Preparation Method on the Formation of True Nimodipine SBE-β-CD/HP-β-CD Inclusion Complexes and Their Dissolution Rates Enhancement

895 | Feb 18 2020

Farouk Semcheddine et al. showed that all the products exhibited higher dissolution rate than those of the physical mixtures and ND alone, in all mediums. However, the kneading complexes displayed the maximum dissolution rate in comparison with drug and other complexes, confirming the influence of the preparation method on the physicochemical properties of the products. [Read the Full Post]

Safety and efficacy of elvitegravir, dolutegravir, and raltegravir in a real-world cohort of treatment-naïve and -experienced patients

789 | Nov 06 2019

Brehm TT et al. showed that side effects were only rarely observed and generally mild in all subgroups. In light of a slightly higher incidence of vertigo and sleep disturbances in patients switched to DTG, awareness of the potential onset of psychiatric symptoms is warranted during follow-up in those patients. [Read the Full Post]

Supramolecular Nanorods of (N-Methylpyridyl) Porphyrin With Captisol: Effective Photosensitizer for Anti-bacterial and Anti-tumor Activitie

455 | Aug 05 2019

Khurana R et al. indicatted that all these synergistic effects of supramolecular nanorods of Captisol-TMPyP complex make the system an effective photosensitizer and a superior antibacterial and antitumor agent. [Read the Full Post]

Associated-Extraction Efficiency of Six Cyclodextrins on Various Flavonoids in Puerariae Lobatae Radix

459 | Jul 05 2019

Feng T et al. indicated that CDs, especially SBE-β-CD, have a promising application for the associated-extraction of flavonoids from PLR. [Read the Full Post]

In Vitro Activity of Sitafloxacin and Additional Newer Generation Fluoroquinolones Against Ciprofloxacin-Resistant Neisseria gonorrhoeae Isolates

412 | Jul 01 2019

Hamasuna R et al. indicated that sitafloxacin should not be considered for empirical first-line monotherapy of gonorrhea. However, sitafloxacin could be valuable in a dual antimicrobial therapy and for cases with ceftriaxone resistance or allergy. [Read the Full Post]

Raltegravir (MK-0518): an integrase inhibitor for the treatment of HIV-1

428 | Jun 20 2019

Evering TH et al. indicated it has demonstrated a favorable side-effect profile in treatment-naive and -experienced patients and a subset of heavy treatment-experienced patients have been able a achieve virologic suppression with raltegravir as part of combination therapy despite limited treatment options. [Read the Full Post]

Puromycin reaction for the A site-bound peptidyl-tRNA

445 | Jun 16 2019

Semenkov Yu et al. indicated that the transpeptidation reaction per se triggers conformational changes in the ribosomal complex bringing the 3'-end of a newly synthesized peptidyl-tRNA nearer to the peptidyl-site of the peptidyltransferase center. This is detected functionally as the ability of such an A site bound peptidyl-tRNA to react with puromycin. This reaction is highly pronounced at elevated (25 degrees C) temperature but can be hardly detected at 0 degrees C. [Read the Full Post]

In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor

460 | May 28 2019

Kobayashi M et al. demonstrated that S/GSK1349572 would be classified as a next-generation drug in the integrase inhibitor class, with a resistance profile markedly different from that of first-generation integrase inhibitors. [Read the Full Post]

Coformulated bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir with emtricitabine and tenofovir alafenamide, for initial treatment of HIV-1 infection (GS-US-380-1490): a randomised, double-blind, multicentre, phase 3, non-inferiority trial

501 | May 08 2019

Sax PE et al. indicated at 48 weeks, virological suppression with the bictegravir regimen was achieved and was non-inferior to the dolutegravir regimen in previously untreated adults. There was no emergent resistance to either regimen. The fixed-dose combination of bictegravir, emtricitabine, and tenofovir alafenamide was safe and well tolerated compared with the dolutegravir regimen. [Read the Full Post]

MK2206 enhances the cytocidal effects of bufalin in multiple myeloma by inhibiting the AKT/mTOR pathway

484 | Jan 11 2019

Xiang RF et al. suggested that MK2206 significantly enhanced the cytocidal effects of bufalin in MM cells, regardless of the sensitivity to bortezomib, via the inhibition of the AKT/mTOR pathway. The study provided the basis of a promising treatment approach for MM. [Read the Full Post]

Micafungin-Induced Suicidal Erythrocyte Death

539 | Nov 14 2018

Peter T et al. showed effect of Micafungin on annexin-V-binding was not significantly modified by removal of extracellular Ca2+, by PKC inhibitor staurosporine (1 µM), p38 kinase inhibitor SB203580 (2 µM), casein kinase 1α inhibitor D4476 (10 µM) or pancaspase inhibitor zVAD (10 µM). [Read the Full Post]

Smac mimetic with TNF-α targets Pim-1 isoforms and reactive oxygen species production to abrogate transformation from blebbishields

1471 | Oct 29 2018

Jinesh GG et al. demonstrated that Smac mimetic in combination with TNF-α is an ideal candidate to target Pim-1 expression, inhibit ROS production and to block transformation from blebbishields. [Read the Full Post]

Antimicrobial susceptibility testing of rapidly growing mycobacteria isolated in Japan

676 | Oct 28 2018

Hatakeyama S et al. demonstrated the importance of correct identification and antimicrobial susceptibility testing, including the testing of potential new agents, in the management of RGM infections. [Read the Full Post]

Tumor Necrosis Factor Inhibits Spread of Hepatitis C Virus Among Liver Cells, Independent From Interferons

826 | Oct 10 2018

Laidlaw SM et al. found TNF to have antiviral effects independently of, as well as in combination with, IFNs. TNF inhibits HCV infection despite increased HCV envelope glycoprotein-mediated infection of liver cells. These findings contradict those from other studies, which have reported that TNF blocks signal transduction in response to IFNs. The destructive inflammatory effects of TNF must be considered along with its antiviral effects. [Read the Full Post]

PTC725, an NS4B-Targeting Compound, Inhibits a Hepatitis C Virus Genotype 3 Replicon, as Predicted by Genome Sequence Analysis and Determined Experimentally

0 | Oct 09 2018

Graci JD et al. identified previously unreported amino acid substitutions selected by PTC725 treatment which further demonstrate that these compounds target the NS4B first transmembrane region. [Read the Full Post]

Inhibition of Histone Deacetylase Activity Aggravates Coxsackievirus B3-Induced Myocarditis by Promoting Viral Replication and Myocardial Apoptosis

557 | Sep 08 2018

Zhou L et al. found inhibition of HDAC activity enhanced myocardial autophagosome formation, which led to the elevated CVB3 viral replication and ensuing increased myocardial apoptosis. [Read the Full Post]

Hepatitis C Virus NS4B Can Suppress STING Accumulation To Evade Innate Immune Responses

1093 | Aug 13 2018

Yi G et al. showed that 2a/JFH1 NS4B has an additional mechanism to evade STING signaling through suppressing STING accumulation. [Read the Full Post]

A profiling study of a newly developed HCVcc strain PR63cc's sensitivity to direct-acting antivirals

1136 | Aug 12 2018

Tao W et al. showed that PR63cc was more resistant than JFH1 to the asunaprevir/daclatasvir combination treatment. In summary, our study systemically analyzed the DAA sensitivity of a new HCVcc strain and identified critical RAVs. These results are not only important for monitoring the emergence of drug-resistant mutations of current DAA therapies, but also valuable for developing next-generation DAAs. [Read the Full Post]

A simple and cost-saving phenotypic drug susceptibility testing of HIV-1

1393 | Jul 05 2018

Weng Y et al. provided a useful tool for interpreting meaningful genotypic mutations and guiding tailored antiviral treatment of HIV/AIDS in clinical practice. [Read the Full Post]

Dissecting the molecular mechanisms that impair stress granule formation in aging cells

1101 | Jul 04 2018

Moujaber O et al. demonstrated that the loss of CReP correlated with the aging-related hyperphosphorylation of eIF2α. Together, we have identified significant changes in the stress response of aging cells and provide mechanistic insights. Based on our work, we propose that the decline in SG formation can provide a new biomarker to evaluate cellular aging. [Read the Full Post]

HMGB1-mediated autophagy decreases sensitivity to oxymatrine in SW982 human synovial sarcoma cells

1197 | May 13 2018

Cai Y et al. showed that combining OMT with an inhibitor of autophagy or HMGB1 may make OMT more effective in the treatment of human synovial sarcoma. [Read the Full Post]

In silico prediction and in vitro and in vivo validation of acaricide fluazuron as a potential inhibitor of FGFR3 and a candidate anticancer drug for bladder carcinoma

814 | Apr 20 2018

Ke K et al. suggested for the first time that fluazuron is a potential inhibitor of FGFR3 and a candidate anticancer drug for the treatment of BC. [Read the Full Post]

Susceptibility of porcine endogenous retrovirus to anti-retroviral inhibitors

720 | Apr 09 2018

Argaw T et al. indicated that some of the licensed anti-retroviral drugs may be useful for controlling PERV infection. However, the efficacy at nanomolar concentrations put forward integrase inhibitors as a drug that has the potential to be useful in the event that xenotransplantation recipients have evidence of PERV transmission and replication. [Read the Full Post]

In Vitro Antibacterial Activity of Rhodanine Derivatives against Pathogenic Clinical Isolates

1267 | Mar 08 2018

AbdelKhalek A et al. suggested that certain rhodanine compounds may have potential use for the treatment of several multidrug-resistant Gram-positive bacterial infections. [Read the Full Post]

Membrane Interactions of Natural Cyclic Lipodepsipeptides of the Viscosin Group.

908 | Feb 18 2018

Geudens N, et al. found that the CLPs interact both with the polar heads and aliphatic tails of model membrane systems, altering bilayer fluidity, while cholesterol reduces CLP insertion depth. [Read the Full Post]

Antibacterial activity and mechanism of action of auranofin against multi-drug resistant bacterial pathogens

1090 | Feb 03 2018

Thangamani S et al. provided valuable evidence that auranofin has significant promise to be repurposed as a novel antibacterial for treatment of invasive bacterial infections. [Read the Full Post]

New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H

936 | Jan 11 2018

Corona A et al. provided new structural information to modulate IN and RNase H inhibitory activities for development of dual-acting anti-HIV agents. [Read the Full Post]

Repurposing auranofin for the treatment of cutaneous staphylococcal infections

1021 | Jan 06 2018

Thangamani S et al. supported that auranofin has potential to be repurposed as a topical antimicrobial agent for the treatment of staphylococcal skin and wound infections. [Read the Full Post]

PTC725, an NS4B-Targeting Compound, Inhibits a Hepatitis C Virus Genotype 3 Replicon, as Predicted by Genome Sequence Analysis and Determined Experimentally.

1398 | Dec 29 2017

Graci JD et al. identified previously unreported amino acid substitutions selected by PTC725 treatment which further demonstrate that these compounds target the NS4B first transmembrane region. [Read the Full Post]

Anidulafungin-Induced Suicidal Erythrocyte Death

0 | Nov 01 2017

Anidulafungin triggers hemolysis and eryptosis with cell shrinkage and phospholipid scrambling of the erythrocyte cell membrane, an effect in part due to Ca2+ entry and activation of p38 kinase. [Read the Full Post]

Ebola VP40 in Exosomes Can Cause Immune Cell Dysfunction

1034 | Sep 24 2017

Dosch JS et al. suggested that the use of drugs such as Oxytetracycline to modulate the levels of exosomes exiting EBOV-infected cells may be able to prevent the devastation of the adaptive immune system and allow for an improved rate of survival. [Read the Full Post]

Cancer stem cell marker phenotypes are reversible and functionally homogeneous in a preclinical model of pancreatic cancer

1550 | Sep 24 2017

Dosch JS, et al. showed that the hierarchical organization of CSCs in human disease is not recapitulated in a commonly used mouse model of pancreatic cancer and therefore provide a new view of the phenotypic and functional heterogeneity of tumor cells. [Read the Full Post]

Antiviral activity of micafungin against enterovirus 71

0 | Aug 05 2017

Kim C et al. identified micafungin, an echinocandin antifungal drug, as a novel inhibitor of EV71. [Read the Full Post]

Cryo-EM reveals a novel octameric integrase structure for betaretroviral intasome function

1260 | Jun 17 2017

Ballandras-Colas A et al. revealed a novel octameric integrase structure for betaretroviral intasome function. [Read the Full Post]

Selectivity for strand-transfer over 3'-processing and susceptibility to clinical resistance of HIV-1 integrase inhibitors are driven by key enzyme-DNA interactions in the active site

1238 | May 13 2017

Métifiot M et al. indicated that the conserved residue Q146 in the flexible loop of HIV-1 integrase is critical for productive viral DNA binding through specific contacts with the virus DNA ends in the 3'-processing and ST reactions. [Read the Full Post]

CD4+ T cell–dependent and –independent cytokine-chemokine network changes in the immune responses of HIV-infected individuals

3580 | Mar 20 2017

Arnold KB et al identified a critical deficiency in NK cell responses of HIV-infected individuals, independent of CD4(+) T cell depletion, which directs secreted profiles. Our findings illustrate a broad approach for identifying key disease-associated nodes in a multicellular, multivariate signaling network. [Read the Full Post]

Solitary inhibition of the breast cancer resistance protein (BCRP) efflux transporter results in a clinically significant drug-drug interaction with rosuvastatin by causing up to a two-fold increase in statin exposure

2464 | Feb 25 2017

Elsby R, et al.'s result shows that solitary inhibition of the intestinal BCRP transporter can result in clinically significant DDIs with rosuvastatin, causing up to a maximum 2-fold increase in exposure, which may warrant statin dose adjustment in clinical practice [Read the Full Post]

Understanding the molecular mechanism of host-based statin resistance in hepatitis C virus replicon containing cells

2213 | Jan 28 2017

Delang L et al. demonstrated that statin resistance in HCV replicon containing hepatoma cells is conferred by changes in the cellular environment. [Read the Full Post]

CD4+ T cell–dependent and –independent cytokine-chemokine network changes in the immune responses of HIV-infected individuals

3700 | Jan 24 2017

Arnold KB, et al. identified a critical deficiency in NK cell responses of HIV-infected individuals, independent of CD4(+) T cell depletion, which directs secreted profiles. Our findings illustrate a broad approach for identifying key disease-associated nodes in a multicellular, multivariate signaling network. [Read the Full Post]

Linking IFNα to apolipoprotein A-I provides a novel therapy of chronic hepadnavirus infection

2400 | Mar 25 2015

Berrondo et al. demonstrated a molecule called InterApo (IA) with IFNα links to apolipoprotein A-I, has antiviral and immunostimulatory activities and lacks IFNα-induced hematological toxicity. In this study, they further explore the safety of IA for chronic HBV infection. [Read the Full Post]

Semen suppresses antiviral activities of microbicides against HIV

2894 | Nov 25 2014

Zirafi et al. reported that microbicides, which can target HIV components, showed ineffective in the presence of semen. [Read the Full Post]

BMS 790052 is the most potent hepatitis C virus inhibitor

4379 | Nov 13 2013

BMS-790052 is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3. [Read the Full Post]

Telaprevir is an associate of a class of antiviral drugs

4499 | Mar 21 2013

Telaprevir is an associate of a class of antiviral drugs called protease inhibitors. Especially, telaprevir prevents the hepatitis C viral enzyme NS3.4A serine protease. Telaprevir is just indicated for use against hepatitis d genotype 1 viral infections and hasnt been which can have an impact on or being protected when employed for other genotypes of the herpes virus. The standard therapy of ribavirin and pegylated interferon is less successful on genotype 1 and a welcome addition is offered by telaprevir to the treatment of this genotype. [Read the Full Post]

Raltegravir is an antiretroviral drug produced by Merck and Co

2834 | Dec 12 2012

Epigenetic marks play a major role in the control of cell fate during mammalian development. Among these, the most studied so far is lysine acetylation, a posttranslational modification of histones which inactivates the positive Raltegravir charge of lysines. [Read the Full Post]

Telaprevir has very poor penetration of the blood brain

5480 | Nov 15 2012

The principal metabolic fate of loperamide in humans involves oxidative N dealkylation to N demethyl loperamide as the principal metabolite. In human liver microsomes, cytochrome P450 3A4 appears to be the major isozyme responsible for loperamide metabolism, with minor contributions from CYP2B6 [Read the Full Post]

BMS-790052 A Tr droplets With twice as many cells pressed

4382 | Oct 23 2012

BMS-790052 A Tr droplets With twice as many cells pressed agA Tr droplets, With twice as many cells pressed against the heart tee h Here cAMP concentration against each other, the proportion of droplets tears reported a positive response [Read the Full Post]

RALTEGRAVIR- AN INTEGRASE INHIBITOR

3494 | Jul 30 2012

HIV-I AND INTEGRASE HIV one of the most tricky viruses on earth that cause immunodeficiency in humans is being studied allot. It is responsible for a deathly disease known AIDS which is a focus of attention of many researchers since last decades. Due to its wide spread and occurrence throughout the world has compelled the scientists to look for a drug that may effectively cure the disease. HIV contains different types of enzymes and genes that help it to utilize the genes and proteins of its host. The most important among all is the integrase enzyme that helps it in integration of its genome into that of the host. Integrase has been an attractive target for the devising a therapy against the disease. A lot of research is being done on integrase inhibitors and several integrase inhibitors have been discovered by high throughput screening that prevent the integration of genome of virus into that of the host hence preventing the proliferation of the host cell. These inhibitors have shown efficacious results when used against HIV-I. One of the examples of such inhibitors is Raltegravir integrase inhibitor. This drug is first of such inhibitors to get FDA approval and is a blessing for the patients of HIV. [Read the Full Post]

RALTEGRAVIR- FAMOUS INTEGRASE INHIBITOR

3848 | Jun 03 2012

INTEGRASE IN CASE OF HIV-1 The most deathly disease on earth, HIV-I, is being researched and studied a lot to find out an effective therapy against it. This virus contains some genes for enzymes/proteins and utilizes some others from the host cells. The enzyme in HIV that helps the virus to integrate its genome into host cell/genome is named as Integrase and gets replicated there. To search for the [roper treatment the first thing that must be keep in mind is resistance development by the mutation of their genes during replication, so it is the need of hour that the research about treatment of cancer must go on further and should be regularly updated. To inhibit their enzymatic activity is an attractive approach. The inhibitors for integrase enzyme have been developed and they inhibit the process of integration of viral genome into the host genome hence prevent its proliferation in the hosting cell. A huge wave of research is going on HIV-I regarding integrase inhibitors that offer promising results against HIV-I virus. Raltegravir integrase inhibitor is such an inhibitor that inhibits the integrase enzyme and it is the first inhibitor to get approved from FDA and its discovery is no doubt considered to be a great blessing. [Read the Full Post]

RALTEGRAVIR- AN INTEGRASE INHIBITOR

3956 | Apr 27 2012

INTEGRASE AND HIV-1 HIV-I, one of the deathly diseases present on earth, is being researched a lot in order to find an efficacious therapy against it. The virus contains some of the genes for proteins/enzymes and utilizes some from the host. Integrase is one of the enzymes present in virus that helps it to integrate its genome into the host genome and get itself replicated there. In order to search for the treatment, first thing that is kept in mind is the development of resistance by getting their genes mutated during replication, therefore it is need of the hour that research on the treatment against cancer must go on and should be updated. Inhibiting the enzymatic activity is one of the approaches. Inhibitors of integrase have also been developed that inhibit the integration of genome of the virus into that of the host and therefore prevent it to proliferate inside the host cell. A lot of research is going on HIV-I in the area of integrase inhibitors which offer new promises in for therapy against HIV-I. Raltegravir integrase inhibitor is one of such inhibitors and the first one to get approval from FDA and the discovery of which is considered a blessing. [Read the Full Post]

RALTEGRAVIR: A POTENT INTEGRASE INHIBITOR

2746 | Apr 01 2012

INTRODUCTION TO HIV-1 AND ITS TREATMENT: HIV-1 is amongst the most destructive viruses and its treatment regime always in a need of more and novel methods to treat this virus because any of the new drugs gives a short time benefit as the virus get resistant against that drug, therefore any of the effective and newly introduced drug is welcomed by the medical practitioners. In order to integrate the genome of virus it needs integrase enzyme, thus inhibitors to this enzyme are potential candidates to inhibit the viral replication inside host cells. For the development and discovery of these inhibitors a lot of work is being done for integrase inhibitors of HIV-1 these inhibitors are also offering new hopes for HIV-1 drugs. Raltegravir integrase inhibitor, first FDA approved HIV integrase inhibitor and the discovery of this inhibitor was much valued. [Read the Full Post]